N,N-二(2-氯乙基)-N'-乙酰基-1,4-苯胺的合成

Synthesis of N,N-bis(2-chloroethyl)-1,4-phenylenediamine

以4-氯硝基苯及二乙醇胺为原料,K_2CO_3为缚酸剂,合成了N,N-二(2-羟基乙基)-4-硝基苯胺,在三乙胺的催化下,利用氯化亚砜将其转化为氮芥关键中间体N,N-二(2-氯乙基)-4-硝基苯胺。在强酸介质中用氯化亚锡将氮芥中间体还原为氮芥类抗肿瘤药效体N,N-二(2-氯乙基)-1,4-苯二胺,以乙酰氯为酰基化试剂,通过酰基化反应合成了芳胺氮芥衍生物N,N-二(2-氯乙基)-N'-乙酰基-1,4-苯胺,并利用元素分析、IR、~1H NMR确证了新化合物的结构。

N,N-bis（2-hydroxy ethyl）-4-nitroaniline using 4-nitrobenzene chloride and diethanolamine as raw materials and K2C03 as HC1 agent. Under the catalysis of triethylamine nitrogen,the main intermedi-ates of N-bis （2-chloroethyl）-4- nitroaniline was synthesized by halogenation agent sulfoxide chloride under the catalysis of strong acid,using reductant stannous chloride synthesizes N,N-bis（2- chloroethyl）- 1,4-phenylenediamine,which is one of nitrogen mustard antitumor efficacy groups,and using the structure of new compounds by elemental analysis, IR,1H NMR pop analysis.